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EP3321271A4 - PROCESS FOR THE PREPARATION OF 7H-PYRROLO [2,3-D] PYRIMIDINE DERIVATIVE AND INTERMEDIATE THEREOF - Google Patents

PROCESS FOR THE PREPARATION OF 7H-PYRROLO [2,3-D] PYRIMIDINE DERIVATIVE AND INTERMEDIATE THEREOF Download PDF

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Publication number
EP3321271A4
EP3321271A4 EP16821437.7A EP16821437A EP3321271A4 EP 3321271 A4 EP3321271 A4 EP 3321271A4 EP 16821437 A EP16821437 A EP 16821437A EP 3321271 A4 EP3321271 A4 EP 3321271A4
Authority
EP
European Patent Office
Prior art keywords
pyrrolo
preparation
pyrimidine derivative
pyrimidine
derivative
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP16821437.7A
Other languages
German (de)
French (fr)
Other versions
EP3321271A1 (en
EP3321271B1 (en
Inventor
Takahiro Yamasaki
Yoshinori Hara
Takayuki Sakai
Kengo Murakami
Katsuyoshi Hara
Naoki Manta
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Japan Tobacco Inc
Original Assignee
Japan Tobacco Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Japan Tobacco Inc filed Critical Japan Tobacco Inc
Publication of EP3321271A1 publication Critical patent/EP3321271A1/en
Publication of EP3321271A4 publication Critical patent/EP3321271A4/en
Application granted granted Critical
Publication of EP3321271B1 publication Critical patent/EP3321271B1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B61/00Other general methods
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Physics & Mathematics (AREA)
EP16821437.7A 2015-07-07 2016-07-06 Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof Active EP3321271B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2015136196 2015-07-07
PCT/JP2016/070046 WO2017006968A1 (en) 2015-07-07 2016-07-06 Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof

Publications (3)

Publication Number Publication Date
EP3321271A1 EP3321271A1 (en) 2018-05-16
EP3321271A4 true EP3321271A4 (en) 2020-12-16
EP3321271B1 EP3321271B1 (en) 2024-05-29

Family

ID=57685105

Family Applications (1)

Application Number Title Priority Date Filing Date
EP16821437.7A Active EP3321271B1 (en) 2015-07-07 2016-07-06 Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof

Country Status (14)

Country Link
US (1) US10822354B2 (en)
EP (1) EP3321271B1 (en)
JP (1) JP6871856B2 (en)
KR (1) KR20180025940A (en)
CN (1) CN107709337B (en)
AU (1) AU2016289061B2 (en)
BR (1) BR112017026173A2 (en)
CA (1) CA2991020A1 (en)
HK (1) HK1251223A1 (en)
IL (1) IL255775B (en)
MX (1) MX2017016772A (en)
RU (1) RU2755618C2 (en)
TW (1) TWI729990B (en)
WO (1) WO2017006968A1 (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
JP2020502224A (en) * 2016-12-21 2020-01-23 日本たばこ産業株式会社 Crystal forms of Janus kinase inhibitors
CN110300756B (en) 2016-12-21 2024-01-02 日本烟草产业株式会社 Preparation method of 7H-pyrrolo[2,3-d]pyrimidine derivatives and its synthetic intermediates
BR112019012267A2 (en) 2016-12-21 2019-12-03 Japan Tobacco Inc Process for the preparation of 7h-pyrrolo [2,3-d] pyrimidine derivative and cocrystals thereof
KR20190105417A (en) 2018-03-05 2019-09-17 현대자동차주식회사 Coupling diagnostic method of breather hose
JP2022526713A (en) 2019-03-21 2022-05-26 オンクセオ Dbait molecule in combination with a kinase inhibitor for the treatment of cancer
CN114173788A (en) * 2019-08-07 2022-03-11 乐敦制药株式会社 Ophthalmic composition for promoting tear secretion
KR20220098759A (en) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) A method of treating cancer that has acquired resistance to a kinase inhibitor
WO2021132598A1 (en) 2019-12-27 2021-07-01 ロート製薬株式会社 Aqueous composition
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111606929B (en) * 2020-06-30 2023-07-07 中瀚(齐河县)生物医药科技有限公司 Preparation method of Degatinib
CN111574540B (en) * 2020-06-30 2023-08-29 云南华派医药科技有限公司 Preparation method of Degatinib
JPWO2022025279A1 (en) 2020-07-30 2022-02-03
EP4176881A4 (en) 2020-07-30 2024-07-31 Rohto Pharmaceutical Co., Ltd. AQUEOUS COMPOSITION
AU2024229918A1 (en) 2023-02-28 2025-09-18 Assia Chemical Industries Ltd. Solid state forms of delgocitinib and process thereof
WO2024225445A1 (en) 2023-04-27 2024-10-31 Japan Tobacco Inc. Crystalline form of delgocitinib

Citations (3)

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ES2335380A1 (en) * 2008-09-24 2010-03-25 Consejo Superior De Investigaciones Cientificas (Cic) NEW QUATERNARY AMINO ACIDS DERIVED FROM AZEPANOS AND ITS APPLICATIONS.
US20110136778A1 (en) * 2009-07-31 2011-06-09 Japan Tobacco Inc. Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof
WO2012098033A1 (en) * 2011-01-19 2012-07-26 Galapagos Nv Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases

Family Cites Families (6)

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US7230119B2 (en) 2004-08-25 2007-06-12 Biocryst Pharmaceuticals, Inc. Process for the preparation of substituted pyrrolidine derivatives and intermediates
DK2078022T3 (en) 2006-09-22 2012-02-13 Janssen Pharmaceutica Nv Spirobenzazepines used as vasopressin antagonists
CN103570601B (en) 2012-07-20 2016-03-30 重庆博腾制药科技股份有限公司 A kind of preparation method of optical active medicine intermediate
DK2964616T3 (en) 2013-03-05 2017-08-28 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
CN110300756B (en) 2016-12-21 2024-01-02 日本烟草产业株式会社 Preparation method of 7H-pyrrolo[2,3-d]pyrimidine derivatives and its synthetic intermediates

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2335380A1 (en) * 2008-09-24 2010-03-25 Consejo Superior De Investigaciones Cientificas (Cic) NEW QUATERNARY AMINO ACIDS DERIVED FROM AZEPANOS AND ITS APPLICATIONS.
US20110136778A1 (en) * 2009-07-31 2011-06-09 Japan Tobacco Inc. Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof
WO2012098033A1 (en) * 2011-01-19 2012-07-26 Galapagos Nv Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DIEGO NÚÑEZ-VILLANUEVA ET AL: "Divergent, stereoselective access to heterocyclic [alpha],[alpha]-quaternary- and [beta] 2,3,3 -amino acid derivatives from a N-Pmp-protected Orn-derived [beta]-lactam", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 13, no. 18, 1 January 2015 (2015-01-01), pages 5195 - 5201, XP055742125, ISSN: 1477-0520, DOI: 10.1039/C5OB00429B *
DIEGO NUNEZ-VILLANUEVA ET AL: "Quaternary a, alpha-2-Oxoazepane a-Amino Acids: Synthesis from Ornithine-Derived beta-Lactams and Incorporation into Model Dipeptides", JOURNAL OF ORGANIC CHEMISTRY, vol. 76, no. 16, 30 June 2011 (2011-06-30), pages 6592 - 6603, XP055605874, ISSN: 0022-3263, DOI: 10.1021/jo200894d.Source: *
PAULA PREZ-FAGINAS ET AL: "Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 19, no. 3, 23 December 2010 (2010-12-23), pages 1155 - 1161, XP028133980, ISSN: 0968-0896, [retrieved on 20101230], DOI: 10.1016/J.BMC.2010.12.052 *
See also references of WO2017006968A1 *

Also Published As

Publication number Publication date
US10822354B2 (en) 2020-11-03
JPWO2017006968A1 (en) 2018-04-19
TWI729990B (en) 2021-06-11
WO2017006968A1 (en) 2017-01-12
HK1251223A1 (en) 2019-01-25
CA2991020A1 (en) 2017-01-12
JP6871856B2 (en) 2021-05-19
AU2016289061A1 (en) 2017-12-21
CN107709337B (en) 2021-11-16
CN107709337A (en) 2018-02-16
KR20180025940A (en) 2018-03-09
AU2016289061B2 (en) 2020-07-09
BR112017026173A2 (en) 2018-08-14
MX2017016772A (en) 2018-05-14
IL255775B (en) 2021-03-25
RU2018104347A3 (en) 2019-12-23
RU2755618C2 (en) 2021-09-17
US20190062346A1 (en) 2019-02-28
EP3321271A1 (en) 2018-05-16
TW201708231A (en) 2017-03-01
RU2018104347A (en) 2019-08-08
EP3321271B1 (en) 2024-05-29
IL255775A (en) 2018-01-31

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